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脂质微球 (LM)在组织分布上与脂质体相似 ,可以选择性地在肿瘤及炎症部位蓄积 ,改变了药物的体内生物分布。研究表明 ,与抗肿瘤药 1,3 双 ( 2 氯乙基 ) 1 亚硝基脲(BCNU)溶液剂相比 ,BCNU LM制剂体外被肿瘤细胞摄取明显增加 ,体内抗肿瘤活性显著增强 ,毒性降低。非甾体抗炎药氟比洛芬易引起胃粘膜损伤等副作用 ,将氟比洛芬乙酸乙酯前药制成LM制剂 ,临床试验表明 ,与药物口服剂型相比 ,LM制剂起效快 ,可迅速止痛 ,不良反应发生率低 ,该制剂已在日本上市。另外 ,还讨论了影响LM分散系稳定性的各种因素。
Lipid microspheres (LM) are similar to liposomes in tissue distribution and may selectively accumulate in tumor and inflammation sites, altering the in vivo biodistribution of drugs. The results showed that compared with the antitumor drug 1,3 bis (2-chloroethyl) 1 nitrosourea (BCNU) solution, the BCNU LM preparation was significantly uptake by tumor cells in vitro and the in vivo antitumor activity was significantly increased and the toxicity was decreased . Non-steroidal anti-inflammatory drug flurbiprofen easily lead to side effects such as gastric mucosal injury, the flurbiprofen ethyl pro-drug made of LM preparations, clinical trials show that, compared with oral drug formulations, LM preparation of rapid onset, Quick analgesic, low incidence of adverse reactions, the preparation has been listed in Japan. In addition, various factors that affect the stability of the LM dispersion are also discussed.